PF-3845

Alias: PF-3845; PF 3845;PF3845;
Cat No.:V0908 Purity: ≥98%
PF-3845 (PF3845; PF 3845) is a novel, biaryl ether piperidine-based, selective and covalent/irreversible inhibitor of FAAH (fatty acid amide hydrolase) with anti-inflammatory, antidiarrheal and antinociceptive effects.
PF-3845 Chemical Structure CAS No.: 1196109-52-0
Product category: FAAH
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PF-3845 (PF3845; PF 3845) is a novel, biaryl ether piperidine-based, selective and covalent/irreversible inhibitor of FAAH (fatty acid amide hydrolase) with anti-inflammatory, antidiarrheal and antinociceptive effects. It inhibits FAAH1 with a Ki of 230 nM, and showed little activity against FAAH2. Structurally, PF-3845 inhibits FAAH by forming a covalent, irreversible bond with the protein, involving carbamylating FAAH's catalytic S241 nucleophile. PF-3845 promotes neuronal survival, attenuates inflammation and improves functional recovery in mice with traumatic brain injury.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In COS-7 cells, PF-3845 (0.5 nM-10 μM; 40 min) exhibits little activity against FAAH-2 (IC50>10 μM) and inhibits human FAAH-1 (IC50=18 nM) in a concentration-dependent manner [1]. Colo-205 cell viability is considerably reduced by PF-3845 (0.1-1000 μM; 48 h)[2].
ln Vivo
In rats, PF-3845 (1–30 mg/kg; po) reduces inflammatory pain in a way that is dependent on cannabinoid receptors[1]. For up to 24 hours, PF-3845 (10 mg/kg; one intraperitoneal; ip) specifically inhibits FAAH in mice[1]. Anandamide (AEA) in mice is dramatically and persistently elevated with administration of PF-3845 (10 mg/kg; single ip)[1].
Animal Protocol
Animal/Disease Models: Male SD (Sprague-Dawley) rats (200g- 250g) are injected CFA[1]
Doses: 1, 3, 10, 30 mg/kg
Route of Administration: Oral administration
Experimental Results: Caused a dose-dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg.
References
[1]. Lamont Booker, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol, 2012, 165(8), 2485-2496.
[2]. Wasilewski A, et, al. Fatty acid amide hydrolase (FAAH) inhibitor PF-3845 reduces viability, migration and invasiveness of human colon adenocarcinoma Colo-205 cell line: an in vitro study. Acta Biochim Pol. 2017;64(3):519-525.
[3]. Ahn K, et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009 Apr 24;16(4):411-20.
[4]. Booker L, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol, 2012, 165(8), 2485-2496.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H23F3N4O2
Molecular Weight
456.46
CAS #
1196109-52-0
SMILES
O=C(N1CCC(CC2=CC=CC(OC3=NC=C(C=C3)C(F)(F)F)=C2)CC1)NC4=CN=CC=C4
Synonyms
PF-3845; PF 3845;PF3845;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 91 mg/mL (199.4 mM)
Water:<1 mg/mL
Ethanol:91 mg/mL (199.4 mM)
Solubility (In Vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 15mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1908 mL 10.9539 mL 21.9077 mL
5 mM 0.4382 mL 2.1908 mL 4.3815 mL
10 mM 0.2191 mL 1.0954 mL 2.1908 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • PF-3845

    Anti-hyperalgesic effects of PF-3845 in the CFA model of inflammatory pain.Chem Biol.2009 Apr 24;16(4):411-20.

  • PF-3845

    In vivo selectivity analysis for PF-3845 and URB597 as determined by competitive ABPP.Chem Biol.2009 Apr 24;16(4):411-20.


  • PF-3845

    Direct analysis of in vivo protein targets of alkyne analogues of PF-3845 and URB597 by CC-ABPP.Chem Biol.2009 Apr 24;16(4):411-20.
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